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MX2011014018A - Pirazincarboxamidas como inhibidores de dgati. - Google Patents

Pirazincarboxamidas como inhibidores de dgati.

Info

Publication number
MX2011014018A
MX2011014018A MX2011014018A MX2011014018A MX2011014018A MX 2011014018 A MX2011014018 A MX 2011014018A MX 2011014018 A MX2011014018 A MX 2011014018A MX 2011014018 A MX2011014018 A MX 2011014018A MX 2011014018 A MX2011014018 A MX 2011014018A
Authority
MX
Mexico
Prior art keywords
sub
alkyl
fluoro
chloro
dgat1
Prior art date
Application number
MX2011014018A
Other languages
English (en)
Inventor
Clive Green
Alan Martin Birch
Paul Michael Murray
Andrew Leach
Leonie Campbell
Roger John Butlin
Michael James Waring
Per Olof Ryberg
Original Assignee
Astrazeneca Ab
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Astrazeneca Ab filed Critical Astrazeneca Ab
Publication of MX2011014018A publication Critical patent/MX2011014018A/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D241/24—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Diabetes (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Se describen compuestos inhibidores de DGAT1 de fórmula (I), sus sales y profármacos aceptables farmacéuticamente, junto con composiciones farmacéuticas, procesos para prepararlos y su uso en el tratamiento, por ejemplo, de la obesidad en donde, por ejemplo, r es 0 ó 1 y X1 es alquilo de 1 a 3 átomos de carbono lineal; q es 0 ó 1 y X1 es fluoro, cloro o alquilo de 1 a 3 átomos de carbono; Y1 se selecciona entre fluoro, cloro, bromo, ciano, alquilo de 1 a 3 átomos de carbono y alcoxi de 1 a 2 átomos de carbono; n es O , 1 ó 2 e Y2 es fluoro, cloro o alquilo de 1 a 3 átomos de carbono; p es 0, 1 ó 2 e Y3 es alquilo de 1 a 3 átomos de carbono o forma un anillo cicloalquilo de 3 a 5 átomos de carbono; Z es carboxi o - CONHSO2Me o -CONRbRc, en donde Rb y Rc se seleccionan independientemente, por ejemplo, entre hidrógeno y alquilo de 1 a 4 átomos de carbono o Rb y Rc se enlazan de modo que formen un anillo morfolina o un anillo heterocíclico de 4 a 6 átomos de carbono y, cuando Z es -CONRbRc, los grupos Rb y Rc pueden estar sustituidos opcionalmente con carboxi.
MX2011014018A 2009-06-19 2010-06-17 Pirazincarboxamidas como inhibidores de dgati. MX2011014018A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US21853909P 2009-06-19 2009-06-19
PCT/GB2010/051003 WO2010146395A1 (en) 2009-06-19 2010-06-17 Pyrazine carboxamides as inhibitors of dgat1

Publications (1)

Publication Number Publication Date
MX2011014018A true MX2011014018A (es) 2012-02-22

Family

ID=42357808

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2011014018A MX2011014018A (es) 2009-06-19 2010-06-17 Pirazincarboxamidas como inhibidores de dgati.

Country Status (14)

Country Link
US (2) US8188092B2 (es)
EP (1) EP2443096A1 (es)
JP (1) JP2012530122A (es)
KR (1) KR20120037939A (es)
CN (1) CN102498103A (es)
AR (1) AR077140A1 (es)
AU (1) AU2010261499A1 (es)
BR (1) BRPI1016109A2 (es)
CA (1) CA2764013A1 (es)
MX (1) MX2011014018A (es)
RU (1) RU2011152517A (es)
TW (1) TW201103895A (es)
UY (1) UY32716A (es)
WO (1) WO2010146395A1 (es)

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TWI644899B (zh) 2013-02-04 2018-12-21 健生藥品公司 Ｆｌａｐ調節劑
US9745328B2 (en) 2013-02-04 2017-08-29 Janssen Pharmaceutica Nv Flap modulators
CN103467392B (zh) * 2013-10-09 2016-08-17 重庆工商大学 一种多卤代吡嗪甲酰胺衍生物及其盐类、制备方法和用途
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Also Published As

Publication number Publication date
UY32716A (es) 2011-01-31
US20120289520A1 (en) 2012-11-15
BRPI1016109A2 (pt) 2016-05-17
KR20120037939A (ko) 2012-04-20
AR077140A1 (es) 2011-08-03
US8188092B2 (en) 2012-05-29
CA2764013A1 (en) 2010-12-23
WO2010146395A1 (en) 2010-12-23
RU2011152517A (ru) 2013-07-27
AU2010261499A1 (en) 2012-01-12
TW201103895A (en) 2011-02-01
JP2012530122A (ja) 2012-11-29
EP2443096A1 (en) 2012-04-25
CN102498103A (zh) 2012-06-13
US20100324068A1 (en) 2010-12-23

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